A selective inhibitor of CSF1R
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BLZ-945

Item No. 19626

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[2-[[(1R,2R)-2-hydroxycyclohexyl]amino]-6-benzothiazolyl]oxy]-N-methyl-2-pyridinecarboxamide
CAS Number
953769-46-5
Molecular Formula
C20H22N4O3S
Formula Weight
398.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mLDMF:PBS (pH 7.2) (1:8): 0.1 mg/mLDMSO: 15 mg/mLEthanol: 1 mg/mL
λmax
229, 273 nm
SMILES
O=C(NC)C1=CC(OC2=CC(SC(N[C@@H]3CCCC[C@H]3O)=N4)=C4C=C2)=CC=N1
InChi Code
InChI=1S/C20H22N4O3S/c1-21-19(26)16-10-13(8-9-22-16)27-12-6-7-15-18(11-12)28-20(24-15)23-14-4-2-3-5-17(14)25/h6-11,14,17,25H,2-5H2,1H3,(H,21,26)(H,23,24)/t14-,17-/m1/s1
InChi Key
ADZBMFGQQWPHMJ-RHSMWYFYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $76

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    10 mg

    $110

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    25 mg

    $241

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    Product Description

    BLZ-945 is a selective inhibitor of the colony stimulating factor 1 receptor (CSF1R) with an IC50 value of 1 nM.1 It is more than 1,000-fold selective against its closest receptor tyrosine kinase homologs.1 It has been shown to inhibit CSF1-dependent proliferation with an EC50 value of 67 nM in bone marrow-derived macrophages.1 In glioma-bearing mice, CSF1R inhibition via BLZ-945 can block tumor progression and significantly improve survival.1 At 200 mg/kg, BLZ-945 decreased the growth of malignant cells in a mouse mammary tumor virus-driven polyomavirus middle T antigen model of mammary carcinogenesis and in a keratin 14-expressing human papillomavirus type 16 transgenic model of cervical carcinogenesis.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pyonteck, S.M., Akkari, L., Schuhmacher, A.J., et al. CSF-1R inhibition alters macrophage polarization and blocks glioma progression. Nat Med. 19(10), 1264-1272 (2013).

    2. Strachan, D.C., Ruffell, B., Oei, Y., et al. CSF1R inhibition delays cervical and mammary tumor growth in murine models by attenuating the turnover of tumor-associated macrophages and enhancing infiltration by CD8+ T cells. Oncoimmunology 2(12), (2013).